Lodoxamide is an ophthalmic mast cell stabilizer that inhibits allergic hypersensitivity reactions. It is used in the treatment of ocular inflammatory states such as vernal conjunctivitis, vernal keratitis, or vernal keratoconjunctivitis. Lodoxamide does not possess antihistaminic or antiinflammatory activity. Lodoxamide (Alomide 0.1%) ophthalmic solution was approved by the FDA in September 1993.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Ophthalmic Administration
-Lodoxamide is for ophthalmic use only.
-Instruct patient on proper instillation of the eye solution.
-Wash hands before and after use.
-Care should be taken to avoid contamination. Do not touch the tip of the dropper to the eye, fingertips, or other surface.
-To avoid contamination or the spread of infection, do not use dropper for more than one person.
During clinical studies of lodoxamide, the most frequently reported adverse reaction was ocular irritation (reported as transient burning, stinging, or discomfort) upon instillation, which occurred in approximately 15% of the subjects.
Lodoxamide ocular adverse events occurring in 1 to 5% of patients included ocular pruritus/itching, blurred vision, dry eyes (xerosis), tearing/discharge (lacrimation), hyperemia, crystalline deposits, and foreign body sensation.
Adverse reactions that occurred with lodoxamide use in less than 1% of the subjects included corneal erosion/ulcer, scales on lid/lash, ocular pain, ocular edema/swelling, ocular warming sensation, ocular fatigue, chemosis, corneal abrasion, anterior chamber cells, keratopathy/keratitis, blepharitis, allergy, sticky sensation, and epitheliopathy.
Nonocular events reported with lodoxamide were headache (1.5%) and (at less than 1%) heat sensation, dizziness, somnolence/drowsiness, nausea, abdominal pain/discomfort, sneezing, dry nose, and rash (unspecified).
Lodoxamide use is contraindicated in any patient with a known lodoxamide hypersensitivity or any of the product components.
Lodoxamide ophthalmic preparation contains benzalkonium chloride as a preservative. As with all other ophthalmic preparations that contain benzalkonium chloride, patients should be instructed not to wear soft contact lenses during treatment with lodoxamide.
Safety and efficacy of lodoxamide has not been established in neonates, infants and children less than two years of age.
There are no adequate and well-controlled studies of lodoxamide use in pregnant women. However, ophthalmic administration of the drug does not result in detectable levels in the plasma and therefore use of the drug during pregnancy would not be expected to cause significant exposure to the fetus. Orally administered lodoxamide at doses of 100 mg/kg/day (1,000 times the proposed human clinical dose) was not associated with any developmental toxicity in rats and rabbits. According to the manufacturer, lodoxamide should be used during pregnancy only if clearly needed.
It is unknown whether lodoxamide is excreted in human milk. However, ophthalmic administration does not result in detectable levels in the plasma and therefore use of the drug during breast-feeding would not be expected to cause significant exposure to the nursing infant. To minimize the amount of drug that reaches systemic circulation, apply pressure over the tear duct in the corner of the eye for 1 to 2 minutes after ophthalmic administration. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, health care providers are encouraged to report the adverse effect to the FDA.
For the treatment of ocular inflammatory states such as vernal conjunctivitis, vernal keratitis, or vernal keratoconjunctivitis:
Ophthalmic dosage:
Adults, Adolescents and Children >= 2 years: 1 to 2 drops in affected eye(s) 4 times per day; not to be used for longer than 3 months.
Neonates, Infants and Children < 2 years: Safety and efficacy have not been established.
Maximum Dosage Limits:
-Adults
8 drops/day per affected eye.
-Geriatric
8 drops/day per affected eye.
-Adolescents
8 drops/day per affected eye.
-Children
>= 2 years: 8 drops/day per affected eye.
< 2 years: Safety and efficacy have not been established.
-Infants
Safety and efficacy have not been established.
-Neonates
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
There are no drug interactions associated with Lodoxamide products.
Lodoxamide is an ophthalmic mast cell stabilizer that inhibits type I immediate hypersensitivity reactions; it inhibits the increases in cutaneous vascular permeability associated with reagin or IgE and antigen-mediated reactions. In vitro studies have demonstrated the ability of lodoxamide to stabilize rodent mast cells and prevent antigen-stimulated release of histamine. In addition, lodoxamide prevents the release of other mast cell inflammatory mediators (e.g., SRS-A, slow-reacting substances of anaphylaxis, also known as the peptidoleukotrienes) and inhibits eosinophil chemotaxis. Although lodoxamide's precise mechanism of action is unknown, the drug has been reported to prevent calcium influx into mast cells upon antigen stimulation. Lodoxamide has no intrinsic vasoconstrictor, antihistaminic, cyclooxygenase inhibition, or other anti-inflammatory activity.
Lodoxamide is administered via ophthalmic administration.
-Route-Specific Pharmacokinetics
Oral Route
The disposition of 14C-lodoxamide was studied in six healthy adult volunteers receiving a 3 mg (50 mCi) oral dose of lodoxamide. Urinary excretion was the major route of elimination. The elimination half-life of 14C-lodoxamide was 8.5 hours in urine.
Other Route(s)
Ophthalmic
In twelve healthy adult volunteers, ophthalmic administration of lodoxamide tromethamine 0.1% solution at a dose of one drop in each eye four times per day for ten days did not result in any measurable plasma concentrations (detection limit = 2.5 ng/mL).